BIIB021

Catalog No.S1175 Synonyms: CNF2024

For research use only.

BIIB021 (CNF2024) is an orally available, fully synthetic small-molecule inhibitor of HSP90 with Ki and EC50 of 1.7 nM and 38 nM, respectively. Phase 2.

BIIB021 Chemical Structure

CAS No. 848695-25-0

Selleck's BIIB021 has been cited by 27 publications

Purity & Quality Control

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Biological Activity

Description BIIB021 (CNF2024) is an orally available, fully synthetic small-molecule inhibitor of HSP90 with Ki and EC50 of 1.7 nM and 38 nM, respectively. Phase 2.
Targets
HSP90 [1]
(Cell-free assay)
1.7 nM(Ki)
In vitro

BIIB021 binds in the ATP-binding pocket of Hsp90, interferes with Hsp90 chaperone function, and results in client protein degradation and tumor growth inhibition. BIIB021 inhibits tumor cell (BT474, MCF-7, N87, HT29, H1650, H1299, H69 and H82) proliferation with IC50 from 0.06-0.31 μM. BIIB021 induces the degradation of Hsp90 client proteins including HER-2, Akt, and Raf-1 and up-regulated expression of the heat shock proteins Hsp70 and Hsp27. [1] BIIB021 inhibits Hodgkin's lymphoma cells (KM-H2, L428, L540, L540cy, L591, L1236 and DEV) with IC50 from 0.24-0.8 μM. BIIB021 shows low activity in lymphocytes from healthy individuals. BIIB021 inhibits the constitutive activity of NF-κB despite defective IκB. BIIB021 induces the expression of ligands for the activating NK cell receptor NKG2D on Hodgkin's lymphoma cells resulting in an increased susceptibility to NK cell–mediated killing. [2] BIIB021 enhanced the in vitro radiosensitivity of HNSCCA cell lines (UM11B and JHU12) with a corresponding reduction in the expression of key radioresponsive proteins, increased apoptotic cells and enhance G2 arrest. [3] BIIB021 is considerably more active than 17-AAG against adrenocortical carcinoma H295R, both in vitro and in vivo. The cytotoxic activity of BIIB021 is not influenced by loss of NQO1 or Bcl-2 overexpression, molecular lesions that do not prevent client loss but are nonetheless associated with reduced cell killing by 17-AAG. BIIB021 is also active in 17-AAG resistant cell lines (NIH-H69, MES SA Dx5, NCI-ADR-RES, Nalm6 and etc.). [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MCF7 MmDnSpVv[3Srb36gZZN{[Xl? NWrqWFR4UW6qaXLpeIlwdiCxZjDIV3A6OC2vZXTpZZRm\CClbHnlcpQheHKxdHXpckBJTVJ{IHTl[5Ji\GG2aX;uJIlvKGi3bXHuJG1ETjdiY3XscJMtKEmFNUC9NE4xOzkQvF2= M3;jSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyMEW1OFI2Lz5{MEC1OVQzPTxxYU6=
BT474 NF7sV5FHfW6ldHnvckBie3OjeR?= MXnCbY5lcW6pIHHm[olvcXS7IITvJGh{eDlyIH71Z4xmd3SrZHWgZolv\GmwZzDkc41icW5iaX6gbJVu[W5iQmS0O|Qh[2WubIOsJGlEPTB;MD6xOO69VQ>? MmnkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB4MEi3N|goRjJyNkC4O|M5RC:jPh?=
MCF7 M3LD[mZ2dmO2aX;uJIF{e2G7 M3vPfWlvcGmkaYTpc44hd2ZiSGPQPVBidHCqYTDpckBpfW2jbjDNR2Y4KGOnbHzzJIF{e2W|c3XkJIF{KGSnZ4Lh[IF1cW:wIH;mJGhmei1{LDDFR|UxRTBwMEO4{txO MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjl|OECzNEc,OjJ7M{iwN|A9N2F-
NCI-H295 NXXxNllIS3m2b4TvfIlkcXS7IHHzd4F6 MlH2NVIxKG2pL3vn M{PYO|Uh\GG7cx?= M3\BN2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG5EUS2KMkm1JINmdGy|IH;2[ZJmgHC{ZYPzbY5oKFCJUDD4[Y5w\3KjZoTl[EBqdiCjdHj5cYlkKG2xdYPlJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[geJVud3JiZ4Lve5RpKGG2IEGyNEBu\y:tZzygdI8heWRiZn;yJFUh\GG7czDw[ZIhf2WnazDmc5IhPCC5ZXXrdy=> MoPPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ7M{iwN|AoRjJ{OUO4NFMxRC:jPh?=
Sf9 NIHE[FFHfW6ldHnvckBie3OjeR?= M33k[lMhcHK| MnnSRolv\GmwZzDh[oZqdmm2eTD0c{BpfW2jbjDOMZRmem2rbnHsJJBwdHmKaYOteIFo\2WmIFjTVFkx[WyyaHGgLGQ6KHSxIFWyN|YqKGGucHjhMYhmdGm6IHPvcoZwem2jdHnvckBmgHC{ZYPz[YQhcW5iaX7z[YN1KHOoOTDj[YxteyCjZoTldkA{KGi{czDifUBndHWxcnXzZ4Vv[2VicH;sZZJqgmG2aX;uJIF{e2G7LDDLbV0xNjByMt88US=> MoPQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|M{K0PFgoRjJ2M{OyOFg5RC:jPh?=
Sf9 Ml7tSpVv[3Srb36gZZN{[Xl? MVizJIhzew>? NFfnWldDcW6maX7nJIFn\mmwaYT5JJRwKGi3bXHuJG4ufGW{bXnuZYwheG:ueVjpd{11[WepZXSgTHNRQTCkZYThJEhFQSC2bzDFNlM3MSCneIDy[ZN{\WRiaX6gbY5{\WO2IIPmPUBk\WyuczDh[pRmeiB|IHjyd{BjgSCobIXvdoV{[2WwY3WgdI9t[XKrenH0bY9vKGG|c3H5MEBMcT1yLkCwOO69VQ>? MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN|MkS4PEc,OjR|M{K0PFg9N2F-
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NB1643 Mn:wdWhVWyCjc4PhfS=> M3vEdZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQkG2OFMh[2WubIO= MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
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OHS-50 M3v6TpFJXFNiYYPzZZk> NVjNToFGeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF;IV{02OCClZXzsdy=> M2PUSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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HCT116 MVXBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NIL6Wmc1QCCqcoO= NEC4S4NCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{Bi\nSncjC0PEBpenNiYomgd5Vt\m:{aH;kZY1qdmViQjDhd5NigSxiR1m1NF0xNjF3zszN NUT1b41QRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1Olc1PTlpPkK5OVY4PDV7PD;hQi=>
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HL60 MU\GeY5kfGmxbjDhd5NigQ>? MmrLNUB2VQ>? NXzqPWI2OjRiaILz MXjJcohq[mm2aX;uJI9nKEiVUEmwJIlvKGi3bXHuJGhNPjBiY3XscJMh[XO|ZYPz[YQh[XNiZH;3cpJm\3WuYYTpc44hd2ZicHjvd5Bpd3K7bHH0[YQhW1SDVEOg[ZhxemW|c3nvckBifCBzIIXNJIFnfGW{IEK0JIhzeyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM> NGXaT2o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUW2O|Q2QSd-Mkm1Olc1PTl:L3G+
HL60 MlfZSpVv[3Srb36gZZN{[Xl? M1;PSlEhfU1? M1HQb|I1KGi{cx?= MlXlTY5pcWKrdHnvckBw\iCKRFHDJIlvKGi3bXHuJGhNPjBiY3XscJMh[XO|ZYPz[YQh[XNidYDy[Yd2dGG2aX;uJI9nKGGlZYT5cE1idHCqYT30eYJ2dGmwIHzleoVteyCjdDCxJJVOKGGodHXyJFI1KGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTV4N{S1PUc,Ojl3Nke0OVk9N2F-
HL60 M{e4T2Z2dmO2aX;uJIF{e2G7 MkTjNUB2VQ>? MmTiNlQhcHK| M3nNVGlvcGmkaYTpc44hd2ZiSFTBR{BqdiCqdX3hckBJVDZyIHPlcIx{KGG|c3Xzd4VlKGG|IIXwdoVofWyjdHnvckBw\iCjY3X0fYxifGWmIHjpd5RwdmViSEOgcIV3\Wy|IHH0JFEhfU1iYX\0[ZIhOjRiaILzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?= M4TINVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NU[3OFU6Lz5{OUW2O|Q2QTxxYU6=
MCF7 NUXtPHhOSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NYiwfpRsSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzMEBKSzVyPUCuN|HPxE1? MkWyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzF4NkO3N|YoRjNzNk[zO|M3RC:jPh?=
In vivo Oral administration of BIIB021 leads to tumor growth inhibition in many tumor xenograft models including N87, BT474, CWR22, U87, SKOV3 and Panc-1. [1] BIIB021 effectively inhibits growth of L540cy tumor at a dose of 120 mg/kg. [2] BIIB021 significantly enhances antitumor growth effect of radiation in JHU12 xenograft. [3]

Protocol (from reference)

Kinase Assay:[1]
  • Hsp90 Binding Assay:

    For fluorescence polarization competition measurements, the FITC-geldanamycin probe (20 nM) is reduced with 2 mM TCEP at room temperature for 3 hours, after which the solution is aliquoted and stored at -80 °C until used. Recombinant human Hsp90α (0.8 nM) and reduced FITC-geldanamycin (2 nM) are incubated in a 96-well microplate at room temperature for 3 hours in the presence of assay buffer containing 20 mM HEPES (pH 7.4), 50 mM KCl, 5 mM MgCl2, 20 mM Na2MoO4, 2 mM DTT, 0.1 mg/mL BGG, and 0.1% (v/v) CHAPS. Following this preincubation, BIIB021 in 100% DMSO is then added to final concentrations of 0.2 nM to 10 μM (final volume 100 μL, 2% DMSO). The reaction is incubated for 16 hours at room temperature and fluorescence is then measured in an Analyst plate reader, excitation = 485 nm, emission = 535 nm. High and low controls contained no BIIB021 or no Hsp90, respectively. The data are fit to a four-parameter curve and IC50 is generated.

Cell Research:[1]
  • Cell lines: BT474, MCF-7, N87, HT29, H1650, H1299, H69 and H82 cells
  • Concentrations: 3 nM - 1 μM
  • Incubation Time: 5 days
  • Method: A modified tetrazolium salt assay is used to measure the IC50. Tumor cells are added to 96-well plates and propagated for 24 hours before BIIB021 addition. BIIB021 is added to the plated cells. DMSO (0.03-0.003%) is included as a vehicle control. After incubation phenazine methosulfate (stock concentration 1 mg/mL) and 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium, inner salt (stock concentration 2 mg/mL) are mixed at a ratio of 1:20 and added to each well of a 96-well plate. Reduction of 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium, inner salt gives rise to a soluble formazan product that is secreted into the culture medium. After 4 hours incubation, the formazan product is quantitated spectrophotometrically at a wavelength of 490 nm. Data are acquired using SOFTmaxPRO software, and 100% viability is defined as the A490 of DMSO-treated cells stained with 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium, inner salt (the mean A490 of cells treated with DMSO at a range of 0.03-0.003%). Percent viability of each sample is calculated from the A490 values as follows: % viability = (A490 nm sample / A490 nm DMSO-treated cells × 100). The IC50 is defined as the concentration that gives rise to 50% inhibition of cell viabilit
Animal Research:[1]
  • Animal Models: N87, BT474, CWR22, U87, SKOV3 and Panc-1 tumor models in BALB/c and athymic mice
  • Dosages: 31, 62.5, and 125 mg/kg
  • Administration: Orally administered once daily

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
30% propylene glycol, 5% Tween 80, 65% D5W
For best results, use promptly after mixing.

30 mg/mL

Chemical Information

Molecular Weight 318.76
Formula

C14H15ClN6O

CAS No. 848695-25-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CN=C(C(=C1OC)C)CN2C=NC3=C2N=C(N=C3Cl)N

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01017198 Completed Drug: BIIB021 and Food|Drug: BIIB0121 and Antacid Advanced Solid Tumors Biogen November 2009 Phase 1
NCT01004081 Completed Drug: BIIB021|Drug: exemestane (Aromasin) Breast Cancer Biogen November 2009 Phase 2
NCT00618735 Completed Drug: BIIB021 Advanced Solid Tumors Biogen February 2008 Phase 1
NCT00618319 Completed Drug: BIIB021 GIST Biogen February 2008 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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